Peringatan Keamanan

The clinical manifestations of butorphanol overdose are those of opioid drugs in general. The most serious symptoms are hypoventilation, cardiovascular insufficiency, coma, and death.

Butorphanol

DB00611

small molecule approved illicit vet_approved

Deskripsi

A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.

Struktur Molekul 2D

Berat 327.4605
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of butorphanol is about 18 hours. In renally impaired patients with creatinine clearances <30 mL/min the elimination half-life is approximately doubled. After intravenous administration to patients with hepatic impairment, the elimination half-life of butorphanol was approximately tripled.
Volume Distribusi * 305 to 901 L
Klirens (Clearance) * 99 +/- 23 L/h [Young with IV 2 mg] * 82 +/- 21 [Eldery with IV 2 mg]

Absorpsi

Rapidly absorbed after intramuscular injection and peak plasma levels are reached in 20-40 minutes. The absolute bioavailability is 60-70% and is unchanged in patients with allergic rhinitis. In patients using a nasal vasoconstrictor (oxymetazoline) the fraction of the dose absorbed was unchanged, but the rate of absorption was slowed. Oral bioavailability is only 5-17% because of extensive first-pass metabolism.

Metabolisme

Extensively metabolized in the liver. The pharmacological activity of butorphanol metabolites has not been studied in humans; in animal studies, butorphanol metabolites have demonstrated some analgesic activity.

Rute Eliminasi

Butorphanol is extensively metabolized in the liver. Elimination occurs by urine and fecal excretion.

Interaksi Makanan

1 Data
  • 1. Avoid alcohol.

Interaksi Obat

915 Data
Buprenorphine Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
Magnesium sulfate The therapeutic efficacy of Butorphanol can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Butorphanol may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
Orphenadrine Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
Pramipexole Butorphanol may increase the sedative activities of Pramipexole.
Ropinirole Butorphanol may increase the sedative activities of Ropinirole.
Rotigotine Butorphanol may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Butorphanol.
Sodium oxybate The risk or severity of CNS depression can be increased when Butorphanol is combined with Sodium oxybate.
Suvorexant Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol The therapeutic efficacy of Tapentadol can be decreased when used in combination with Butorphanol.
Thalidomide Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Alvimopan The risk or severity of adverse effects can be increased when Butorphanol is combined with Alvimopan.
Desmopressin The risk or severity of hyponatremia can be increased when Butorphanol is combined with Desmopressin.
Pegvisomant The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Butorphanol.
Succinylcholine The risk or severity of bradycardia can be increased when Succinylcholine is combined with Butorphanol.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Butorphanol.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Butorphanol.
Methylnaltrexone Butorphanol may increase the opioid antagonism activities of Methylnaltrexone.
Naloxegol Butorphanol may increase the opioid antagonism activities of Naloxegol.
Mirtazapine Butorphanol may increase the serotonergic activities of Mirtazapine.
Fluvoxamine The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Fluvoxamine.
Citalopram The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Citalopram.
Duloxetine The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Duloxetine.
Paroxetine The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Paroxetine.
Sertraline The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Sertraline.
Sibutramine The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Sibutramine.
Nefazodone The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Nefazodone.
Zimelidine The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Zimelidine.
Dapoxetine The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Dapoxetine.
Milnacipran The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Butorphanol.
Seproxetine The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Seproxetine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Levomilnacipran.
Indalpine The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Indalpine.
Ritanserin The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Ritanserin.
Alaproclate The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Alaproclate.
Ethanol Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Butorphanol may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Butorphanol.
Phentermine Phentermine may increase the analgesic activities of Butorphanol.
Pseudoephedrine Pseudoephedrine may increase the analgesic activities of Butorphanol.
Benzphetamine Benzphetamine may increase the analgesic activities of Butorphanol.
Diethylpropion Diethylpropion may increase the analgesic activities of Butorphanol.
Lisdexamfetamine The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Lisdexamfetamine.
Mephentermine Mephentermine may increase the analgesic activities of Butorphanol.
MMDA MMDA may increase the analgesic activities of Butorphanol.
Midomafetamine Midomafetamine may increase the analgesic activities of Butorphanol.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may increase the analgesic activities of Butorphanol.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may increase the analgesic activities of Butorphanol.
Tenamfetamine Tenamfetamine may increase the analgesic activities of Butorphanol.
Chlorphentermine Chlorphentermine may increase the analgesic activities of Butorphanol.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may increase the analgesic activities of Butorphanol.
Dextroamphetamine Dextroamphetamine may increase the analgesic activities of Butorphanol.
Metamfetamine Metamfetamine may increase the analgesic activities of Butorphanol.
Iofetamine I-123 Iofetamine I-123 may increase the analgesic activities of Butorphanol.
Ritobegron Ritobegron may increase the analgesic activities of Butorphanol.
Mephedrone Mephedrone may increase the analgesic activities of Butorphanol.
Methoxyphenamine Methoxyphenamine may increase the analgesic activities of Butorphanol.
Gepefrine Gepefrine may increase the analgesic activities of Butorphanol.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may increase the analgesic activities of Butorphanol.
Amphetamine Amphetamine may increase the analgesic activities of Butorphanol.
Phendimetrazine Phendimetrazine may increase the analgesic activities of Butorphanol.
Mecamylamine The risk or severity of adverse effects can be increased when Mecamylamine is combined with Butorphanol.
Pentolinium The risk or severity of adverse effects can be increased when Pentolinium is combined with Butorphanol.
Trimethaphan The risk or severity of adverse effects can be increased when Trimethaphan is combined with Butorphanol.
Chloroprocaine The risk or severity of CNS depression can be increased when Butorphanol is combined with Chloroprocaine.
Fenoterol The risk or severity of adverse effects can be increased when Fenoterol is combined with Butorphanol.
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione The risk or severity of adverse effects can be increased when Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione is combined with Butorphanol.
Agmatine The risk or severity of adverse effects can be increased when Agmatine is combined with Butorphanol.
Promazine The risk or severity of adverse effects can be increased when Promazine is combined with Butorphanol.
Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Butorphanol.
Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with Butorphanol.
Promethazine The risk or severity of adverse effects can be increased when Promethazine is combined with Butorphanol.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Butorphanol.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Butorphanol.
Benzatropine The risk or severity of adverse effects can be increased when Benzatropine is combined with Butorphanol.
Disopyramide The risk or severity of adverse effects can be increased when Disopyramide is combined with Butorphanol.
Ipratropium The risk or severity of adverse effects can be increased when Ipratropium is combined with Butorphanol.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Butorphanol.
Terfenadine The risk or severity of adverse effects can be increased when Terfenadine is combined with Butorphanol.
Buclizine The risk or severity of adverse effects can be increased when Buclizine is combined with Butorphanol.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Butorphanol.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Butorphanol.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Butorphanol.
Profenamine The risk or severity of adverse effects can be increased when Profenamine is combined with Butorphanol.
Hyoscyamine The risk or severity of adverse effects can be increased when Hyoscyamine is combined with Butorphanol.
Cyproheptadine The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Butorphanol.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Butorphanol.
Darifenacin The risk or severity of adverse effects can be increased when Darifenacin is combined with Butorphanol.

Target Protein

Kappa-type opioid receptor OPRK1
Delta-type opioid receptor OPRD1
Mu-type opioid receptor OPRM1

Referensi & Sumber

Synthesis reference: Monkovic, I. and Conway, T.T.; U.S. Patent 3,775,414; November 27,1973; Monkovic, I.,Wong, H. and Lim, G.; U.S. Patent 3,980,641; September 14, 1976; Pachter, IJ., Belleau, B.R. and Monkovic, I.; U.S. Patent 3,819,635; June 25,1974; and Lim, G. and Hooper, J.W.; U.S. Patent 4,017,497; April 12,1977; all assigned to Bristol-Myers Company.
Artikel (PubMed)
  • PMID: 10534607
    Gear RW, Miaskowski C, Gordon NC, Paul SM, Heller PH, Levine JD: The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain. Pain. 1999 Nov;83(2):339-45.
  • PMID: 12127012
    Fan LW, Tanaka S, Tien LT, Ma T, Rockhold RW, Ho IK: Withdrawal from dependence upon butorphanol uniquely increases kappa(1)-opioid receptor binding in the rat brain. Brain Res Bull. 2002 Jun;58(2):149-60.

Contoh Produk & Brand

Produk: 34 • International brands: 2
Produk
  • Butorphanol Nasal Spray
    Solution • 10 mg / mL • Nasal • Canada • Approved
  • Butorphanol Tartrate
    Spray • 10 mg/1mL • Nasal • US • Generic • Approved
  • Butorphanol Tartrate
    Spray, metered • 10 mg/1mL • Nasal • US • Generic • Approved
  • Butorphanol Tartrate
    Injection • 1 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
  • Butorphanol Tartrate
    Injection • 2 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
  • Butorphanol Tartrate
    Injection • 2 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
  • Butorphanol Tartrate
    Injection • 2 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
  • Butorphanol Tartrate
    Injection • 1 mg/1mL • Intramuscular; Intravenous • US • Generic • Approved
Menampilkan 8 dari 34 produk.
International Brands
  • Butaro — Lotus Pharmaceuticals
  • Butrum — Aristo

Sekuens Gen/Protein (FASTA)

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